GGTI-2418 - 10mM in DMSO , CAS No.501010-06-6

CAS: 501010-06-6 Cat. No.: G655273 Molecular Weight: 441.5 PubChem CID: 11539477

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

GGTI-2418 is a highly potent, competitive, and selective geranylgeranyltransferase I ( GGTase I ) inhibitor. GGTI-2418 inhibits GGTase I and FTase activities with IC 50 s of 9.5 nM and 53 μM, respectively. GGTI-2418 also increases p27(Kip1) and induces significant regression of breast tumors

In Vitro

GGTI-2418 inhibits GGTase I and FTase activities with IC 50 s of 9.5±2.0 nM and 53±11 μM, respectively, a 5,600-fold selectivity toward inhibition of GGTase I versus FTase. GGTI-2418 demonstrates competitive inhibition of GGTase I against the H-Ras-CVLL protein with a K i of 4.4±1.6 nM. GGTi-2418 (10-15 μM; 16 hours) treatment delocalizes FBXL2 and stabilizes IP3R3. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: HeLa cells Concentration: 10-15 μM Incubation Time: 16 hours Result: Delocalized FBXL2 and stabilized IP3R3.

In Vivo

GGTI-2418 (100 mg/kg daily or 200 mg/kg every third day; 15 days) significantly inhibits the growth of breast tumor xenografts in nude mice with MDA-MB-231 xenografts . GGTI-2418 (100 mg/kg daily; 5 days) induces regression of ErbB2-driven mammary tumors in ErbB2 transgenic mice . GGTI-2418 inhibits the geranylgeranylation of Rap1 and causes a dramatic decrease in S473 phosphorylation of Akt. GGTI-2418 also upregulates p27 levels in vivo . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Nude mice implanted with MDA-MB-231 breast cancer tumors Dosage: 100 mg/kg daily or 200 mg/kg every third day Administration: Injected intraperitoneally; 15 days Result: Inhibited the growth of breast tumor xenografts. Animal Model: ErbB2 transgenic mice Dosage: 100 mg/kg/day Administration: Subcutaneously; 5 days Result: Halted tumor growth and induced massive tumor regression. Tumor decreased by 76% following GGTI-2418 treatment.

IC50& Target:IC50: 9.5 nM (GGTase I), 53 μM (FTase)

Specifications

Specifications & Purity

10mM in DMSO

Biochemical and Physiological Mechanisms

GGTI-2418 is a highly potent, competitive, and selective geranylgeranyltransferase I ( GGTase I ) inhibitor. GGTI-2418 inhibits GGTase I and FTase activities with IC 50 s of 9.5 nM and 53 μM, respectively. GGTI-2418 also increases p27(Kip1) and induces si

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

INHIBITOR

Names and Identifiers

• Isomeric SMILES: CC1=C(N=CN1)CN2CCN([C@H](C2=O)CC3=CC=CC=C3)C(=O)N[C@@H](CC(C)C)C(=O)O
• PubChem CID: 11539477
• Molecular Weight: 441.5